WO2011044185A3 - Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use - Google Patents

Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use Download PDF

Info

Publication number
WO2011044185A3
WO2011044185A3 PCT/US2010/051558 US2010051558W WO2011044185A3 WO 2011044185 A3 WO2011044185 A3 WO 2011044185A3 US 2010051558 W US2010051558 W US 2010051558W WO 2011044185 A3 WO2011044185 A3 WO 2011044185A3
Authority
WO
WIPO (PCT)
Prior art keywords
compounds
heterocyclic compounds
compositions
bace
inhibitors
Prior art date
Application number
PCT/US2010/051558
Other languages
French (fr)
Other versions
WO2011044185A2 (en
Inventor
Ulrich Iserloh
Andrew W. Stamford
Jared N. Cumming
Original Assignee
Schering Corporation
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Schering Corporation filed Critical Schering Corporation
Priority to EP10822570.7A priority Critical patent/EP2485920B1/en
Priority to US13/391,441 priority patent/US8569310B2/en
Publication of WO2011044185A2 publication Critical patent/WO2011044185A2/en
Publication of WO2011044185A3 publication Critical patent/WO2011044185A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/20—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D239/22—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond

Abstract

In its many embodiments, the present invention provides certain pentafluorosulfur imino heterocyclic compounds, including compounds Formula (a) and pharmaceutically acceptable salts thereof. Compounds of Formula(a) have the general structure: (a) wherein each variable is selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimers Disease, are also disclosed.
PCT/US2010/051558 2009-10-08 2010-10-06 Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use WO2011044185A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP10822570.7A EP2485920B1 (en) 2009-10-08 2010-10-06 Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
US13/391,441 US8569310B2 (en) 2009-10-08 2010-10-06 Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions and their use

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US24968609P 2009-10-08 2009-10-08
US61/249,686 2009-10-08

Publications (2)

Publication Number Publication Date
WO2011044185A2 WO2011044185A2 (en) 2011-04-14
WO2011044185A3 true WO2011044185A3 (en) 2012-06-14

Family

ID=43857359

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2010/051558 WO2011044185A2 (en) 2009-10-08 2010-10-06 Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use

Country Status (3)

Country Link
US (1) US8569310B2 (en)
EP (1) EP2485920B1 (en)
WO (1) WO2011044185A2 (en)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8637504B2 (en) 2008-06-13 2014-01-28 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
US8653067B2 (en) 2007-04-24 2014-02-18 Shionogi & Co., Ltd. Pharmaceutical composition for treating Alzheimer's disease
US8691831B2 (en) 2007-02-23 2014-04-08 Merck Sharp & Dohme Corp. Heterocyclic aspartyl protease inhibitors
US9145426B2 (en) 2011-04-07 2015-09-29 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
US9181236B2 (en) 2011-08-22 2015-11-10 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use
US9221839B2 (en) 2011-04-07 2015-12-29 Merck Sharp & Dohme Corp. C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101052122B1 (en) 2005-10-25 2011-07-26 시오노기세야쿠 가부시키가이샤 Aminodihydrothiazine derivatives
AU2008245082B8 (en) 2007-04-24 2012-09-13 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives substituted with a cyclic group
WO2010047372A1 (en) 2008-10-22 2010-04-29 塩野義製薬株式会社 2-aminopyridin-4-one and 2-aminopyridine derivative both having bace1-inhibiting activity
TW201020244A (en) 2008-11-14 2010-06-01 Astrazeneca Ab New compounds
UA108363C2 (en) 2009-10-08 2015-04-27 IMINOTIADIASIADIOXIDE OXIDES AS BACE INHIBITORS, COMPOSITIONS THEREOF AND THEIR APPLICATIONS
WO2011044184A1 (en) * 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
WO2011044185A2 (en) 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
US8563543B2 (en) 2009-10-08 2013-10-22 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2511268B2 (en) 2009-12-11 2021-02-17 Shionogi & Co., Ltd. Oxazine derivative
JP5766198B2 (en) 2010-10-29 2015-08-19 塩野義製薬株式会社 Condensed aminodihydropyrimidine derivatives
CN103261199A (en) 2010-10-29 2013-08-21 盐野义制药株式会社 Naphthyridine derivative
MX2013011947A (en) 2011-04-13 2014-01-16 Merck Sharp & Dohme 5-substituted iminothiazines and their mono-and dioxides as bace inhibitors,compositions,and their use.
WO2012147763A1 (en) 2011-04-26 2012-11-01 塩野義製薬株式会社 Oxazine derivative and bace 1 inhibitor containing same
US9422277B2 (en) 2012-10-17 2016-08-23 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use
US9416129B2 (en) 2012-10-17 2016-08-16 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use
US9540359B2 (en) 2012-10-24 2017-01-10 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having BACE1 inhibitory activity
US8865723B2 (en) 2012-10-25 2014-10-21 Tetra Discovery Partners Llc Selective PDE4 B inhibition and improvement in cognition in subjects with brain injury
EP2931284B1 (en) 2012-12-14 2017-08-23 Merck Sharp & Dohme Corp. Bace inhibitors of iminothiadiazine dioxides
US9489013B2 (en) 2012-12-20 2016-11-08 Merck Sharp & Dohme Corp. C6-azaspiro iminothiadiazine dioxides as bace inhibitors, compositions, and their use
CN104870000A (en) 2012-12-20 2015-08-26 默沙东公司 C5, C6 oxacyclic-fused iminothiazine dioxide compounds as BACE inhibitors
EP2934534B1 (en) * 2012-12-21 2017-12-13 Merck Sharp & Dohme Corp. C5-spiro iminothiadiazine dioxides as bace inhibitors
US9957269B2 (en) 2014-09-12 2018-05-01 Merck Sharp & Dohme Corp. S-imino-S-oxo iminothiazine compounds as bace inhibitors, compositions, and their use
WO2016044120A1 (en) 2014-09-19 2016-03-24 Merck Sharp & Dohme Corp. Diazine-fused amidine compounds as bace inhibitors, compositions, and their use
EP3383493B1 (en) 2015-12-04 2021-02-17 Merck Sharp & Dohme Corp. Carbocyclic fused iminothiadiazine dioxides as bace inhibitors, compositions, and their use

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070287692A1 (en) * 2006-06-12 2007-12-13 Yusheng Wu Aspartyl protease inhibitors

Family Cites Families (106)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1990004197A1 (en) 1988-10-07 1990-04-19 Eastman Kodak Company Camera view finder
US5534520A (en) 1990-04-10 1996-07-09 Fisher; Abraham Spiro compounds containing five-membered rings
AU2436792A (en) 1991-08-16 1993-03-16 Merck & Co., Inc. Quinazoline derivatives as inhibitors of hiv reverse transcriptase
AU3704400A (en) * 1999-03-04 2000-09-21 E.I. Du Pont De Nemours And Company Fused bicyclic oxazinone and thiazinone fungicides
US7161962B1 (en) 1999-05-27 2007-01-09 Nuera Communications, Inc. Method and apparatus for coding modem signals for transmission over voice networks
PL372212A1 (en) 2001-08-03 2005-07-11 Schering Corporation Novel gamma secretase inhibitors
GB0211649D0 (en) 2002-05-21 2002-07-03 Novartis Ag Organic compounds
US7244764B2 (en) 2003-06-23 2007-07-17 Neurochem (International) Limited Methods and compositions for treating amyloid-related diseases
CN1863797A (en) 2003-08-08 2006-11-15 先灵公司 Cyclic amine BACE-1 inhibitors having a benzamide substituent
TW200524910A (en) 2003-08-08 2005-08-01 Schering Corp Cyclic amine BACE-1 inhibitors having a heterocyclic substituent
US20060034848A1 (en) 2003-11-07 2006-02-16 Ayae Kinoshita Methods and compositions for treating Alzheimer's disease
EP2343069B1 (en) * 2003-12-15 2016-03-02 Merck Sharp & Dohme Corp. Heterocyclic aspartyl protease inhibitors
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
JP2008503459A (en) 2004-06-16 2008-02-07 ワイス Amino-5,5-diphenylimidazolone derivatives for inhibiting β-secretase
RU2006144075A (en) 2004-06-16 2008-07-27 Вайет (Us) DIPHENYLIMIDAZOPYRIMIDINE AND β-IMIDAZOLAMINES AS β-SECRETASE INHIBITORS
US7803802B2 (en) 2004-07-22 2010-09-28 Schering Corporation Substituted amide beta secretase inhibitors
WO2006014944A1 (en) 2004-07-28 2006-02-09 Schering Corporation Macrocyclic beta-secretase inhibitors
US20090062282A1 (en) 2004-10-15 2009-03-05 Astrazeneca Ab Substituted Amino-Pyrimidones and Uses Thereof
US20090221579A1 (en) 2004-10-15 2009-09-03 Jeffrey Scott Albert Substituted Amino-Compounds and Uses Thereof
DE102005023943A1 (en) 2005-05-20 2006-11-23 Grünenthal GmbH Pentafluorosulfanyl-substituted compound and its use for the preparation of medicaments
US7759353B2 (en) 2005-06-14 2010-07-20 Schering Corporation Substituted spiro iminopyrimidinones as aspartyl protease inhibitors, compositions, and methods of treatment
MX2007016185A (en) 2005-06-14 2008-03-07 Schering Corp Macrocyclic heterocyclic aspartyl protease inhibitors.
CA2609582A1 (en) 2005-06-14 2006-12-28 Schering Corporation Aspartyl protease inhibitors
CN101198597B (en) 2005-06-14 2011-11-16 先灵公司 Preparation and use of compounds as aspartyl protease inhibitors
WO2006138265A2 (en) 2005-06-14 2006-12-28 Schering Corporation Heterocyclic aspartyl protease inhibitors, preparation and use thereof
WO2006138230A2 (en) 2005-06-14 2006-12-28 Schering Corporation The preparation and use of protease inhibitors
MX2007016175A (en) 2005-06-14 2008-03-07 Schering Corp Aspartyl protease inhibitors.
TW200738683A (en) 2005-06-30 2007-10-16 Wyeth Corp Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation
AU2006266167A1 (en) 2005-06-30 2007-01-11 Wyeth Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for beta-secretase modulation
TW200730523A (en) 2005-07-29 2007-08-16 Wyeth Corp Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation
WO2007038271A1 (en) 2005-09-26 2007-04-05 Wyeth Amino-5- [4- (difluoromethoxy) phenyl] -5-phenylimidazolone compounds as inhibitors of the beta-secretase (bace)
KR101052122B1 (en) 2005-10-25 2011-07-26 시오노기세야쿠 가부시키가이샤 Aminodihydrothiazine derivatives
JP2009513656A (en) 2005-10-27 2009-04-02 シェーリング コーポレイション Heterocyclic aspartyl protease inhibitors
JP2009513670A (en) 2005-10-31 2009-04-02 シェーリング コーポレイション Aspartyl protease inhibitor
WO2007058581A1 (en) 2005-11-15 2007-05-24 Astrazeneca Ab Novel 2-aminopyrimidine derivatives and their use
JP2009515949A (en) 2005-11-15 2009-04-16 アストラゼネカ・アクチエボラーグ Novel 2-aminopyrimidinone derivatives and their use
AR058381A1 (en) 2005-12-19 2008-01-30 Astrazeneca Ab COMPOUNDS DERIVED FROM 2-AMINOPIRIDIN-4-ONAS AND A PHARMACEUTICAL COMPOSITION
GB0602951D0 (en) 2006-02-14 2006-03-29 Novartis Ag Organic Compounds
JP2009532464A (en) 2006-04-05 2009-09-10 アストラゼネカ・アクチエボラーグ 2-Aminopyrimidin-4-one and its use for treating or preventing Aβ-related pathologies
TW200815443A (en) 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds I
TW200815449A (en) 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds II
TW200815447A (en) 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds IV
TW200808796A (en) 2006-06-14 2008-02-16 Astrazeneca Ab New compounds III
TW200815349A (en) 2006-06-22 2008-04-01 Astrazeneca Ab New compounds
KR20090087487A (en) 2006-12-12 2009-08-17 쉐링 코포레이션 Aspartyl protease inhibitors
EP2061771A1 (en) 2006-12-12 2009-05-27 Schering Corporation Aspartyl protease inhibitors containing a tricyclic ring system
TW200831484A (en) 2006-12-20 2008-08-01 Astrazeneca Ab New compounds
TW200831091A (en) 2006-12-20 2008-08-01 Astrazeneca Ab New compounds
AU2008245082B8 (en) 2007-04-24 2012-09-13 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives substituted with a cyclic group
JP5383483B2 (en) 2007-04-24 2014-01-08 塩野義製薬株式会社 Pharmaceutical composition for the treatment of Alzheimer's disease
WO2009005470A1 (en) 2007-07-05 2009-01-08 Astrazeneca Ab Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors
US20090041201A1 (en) 2007-08-06 2009-02-12 Carestream Health, Inc. Alignment apparatus for imaging system
CN101910143B (en) 2008-01-18 2013-08-21 卫材R&D管理有限公司 Condensed aminodihydrothiazine derivative
EP2283016B1 (en) 2008-04-22 2014-09-24 Merck Sharp & Dohme Corp. Thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as bace-1 inhibitors, compositions, and their use
TWI431004B (en) 2008-05-02 2014-03-21 Lilly Co Eli Bace inhibitors
US8637504B2 (en) 2008-06-13 2014-01-28 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
EP2324032B1 (en) 2008-08-19 2014-10-01 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
KR20110076965A (en) 2008-09-30 2011-07-06 에자이 알앤드디 매니지먼트 가부시키가이샤 Novel fused aminodihydrothiazine derivative
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
WO2010047372A1 (en) 2008-10-22 2010-04-29 塩野義製薬株式会社 2-aminopyridin-4-one and 2-aminopyridine derivative both having bace1-inhibiting activity
WO2010063718A1 (en) 2008-12-02 2010-06-10 ETH Zürich Screening assay for metabolic disease therapeuticals
WO2010113848A1 (en) 2009-03-31 2010-10-07 塩野義製薬株式会社 Isothiourea derivative or isourea derivative having bace1 inhibitory activity
AR077277A1 (en) 2009-07-09 2011-08-17 Lilly Co Eli BICYCLE COMPOUNDS (1,3) TIAZIN-2-AMINA PHARMACEUTICAL FORMULATION THAT INCLUDES IT AND ITS USE FOR THE MANUFACTURE OF A USEFUL MEDICINAL PRODUCT FOR THE TREATMENT OF ALZHEIMER'S DISEASE
GB0912778D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydro-oxazine derivatives
GB0912777D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydropyrimidone derivatives
AR077328A1 (en) 2009-07-24 2011-08-17 Novartis Ag DERIVATIVES OF OXAZINE AND ITS USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS
US8188079B2 (en) 2009-08-19 2012-05-29 Hoffman-La Roche Inc. 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines
UA108363C2 (en) 2009-10-08 2015-04-27 IMINOTIADIASIADIOXIDE OXIDES AS BACE INHIBITORS, COMPOSITIONS THEREOF AND THEIR APPLICATIONS
WO2011044184A1 (en) 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
WO2011044185A2 (en) 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
US8563543B2 (en) * 2009-10-08 2013-10-22 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
CN102686584A (en) 2009-11-13 2012-09-19 盐野义制药株式会社 Aminothiazine or aminooxazine derivative having amino linker
WO2011071057A1 (en) 2009-12-09 2011-06-16 塩野義製薬株式会社 Pharmaceutical composition for treatment or prevention of alzheimer's disease containing sulfur-containing heterocyclic derivative
WO2011070781A1 (en) 2009-12-09 2011-06-16 塩野義製薬株式会社 Substituted aminothiazine derivative
US7964594B1 (en) 2009-12-10 2011-06-21 Hoffmann-La Roche Inc. Amino oxazine derivatives
JPWO2011071109A1 (en) 2009-12-11 2013-04-22 塩野義製薬株式会社 Fused heterocyclic compounds having an amino group
UA103272C2 (en) 2009-12-11 2013-09-25 Ф. Хоффманн-Ля Рош Аг 2-amino-5,5-difluoro-5,6-dihydro-4h-[1,3]oxazines as bace1 and/or bace2 inhibitors
EP2511268B2 (en) 2009-12-11 2021-02-17 Shionogi & Co., Ltd. Oxazine derivative
EP2518059A4 (en) 2009-12-24 2013-05-29 Shionogi & Co 4-amino-1,3-thiazine or oxazine derivative
WO2011142716A1 (en) 2010-05-12 2011-11-17 Astrazeneca Ab Novel hemifumarate salt of isoindole compound acting as bace inhibitor
KR101730937B1 (en) 2010-06-09 2017-04-27 얀센 파마슈티카 엔.브이. 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace)
ES2442905T3 (en) 2010-07-13 2014-02-14 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
JP5766198B2 (en) 2010-10-29 2015-08-19 塩野義製薬株式会社 Condensed aminodihydropyrimidine derivatives
CN103261199A (en) 2010-10-29 2013-08-21 盐野义制药株式会社 Naphthyridine derivative
BR112013017779A2 (en) 2011-01-12 2016-10-11 Novartis Ag oxazine derivatives and their use in the treatment of neurological disorders
US8524897B2 (en) 2011-01-12 2013-09-03 Novartis Ag Crystalline oxazine derivative
WO2012095521A1 (en) 2011-01-13 2012-07-19 Novartis Ag Bace-2 inhibitors for the treatment of metabolic disorders
EP2663561B1 (en) 2011-01-13 2016-03-16 Novartis AG Novel heterocyclic derivatives and their use in the treatment of neurological disorders
US9242943B2 (en) 2011-01-18 2016-01-26 Siena Biotech S.P.A. 1,4 oxazines as BACE1 and/or BACE2 inhibitors
GB201101140D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101139D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
US8399459B2 (en) 2011-02-02 2013-03-19 Hoffmann-La Roche Inc. 1,4 oxazines as BACE1 and/or BACE2 inhibitors
WO2012138590A1 (en) 2011-04-07 2012-10-11 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2694489B1 (en) 2011-04-07 2017-09-06 Merck Sharp & Dohme Corp. C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
US8754075B2 (en) 2011-04-11 2014-06-17 Hoffmann-La Roche Inc. 1,3-oxazines as BACE1 and/or BACE2 inhibitors
MX2013011947A (en) 2011-04-13 2014-01-16 Merck Sharp & Dohme 5-substituted iminothiazines and their mono-and dioxides as bace inhibitors,compositions,and their use.
WO2012147763A1 (en) 2011-04-26 2012-11-01 塩野義製薬株式会社 Oxazine derivative and bace 1 inhibitor containing same
EP2703401A4 (en) 2011-04-26 2014-12-03 Shionogi & Co Pyridine derivative and bace-1 inhibitor containing same
US8785436B2 (en) 2011-05-16 2014-07-22 Hoffmann-La Roche Inc. 1,3-oxazines as BACE 1 and/or BACE2 inhibitors
US9079919B2 (en) 2011-05-27 2015-07-14 Hoffmann-La Roche Inc. Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as BACE1 and/or BACE2 inhibitors
JP2012250933A (en) 2011-06-03 2012-12-20 Shionogi & Co Ltd Pharmaceutical composition containing oxazine derivative for treating or preventing alzheimer's disease
MX2013014007A (en) 2011-06-07 2014-03-12 Hoffmann La Roche [1,3]oxazines.
BR112013031098A2 (en) 2011-06-07 2016-12-06 Hoffmann La Roche haloalkyl-1,3 oxazines as inhibitors of bace1 and / or bace2
AU2012298983A1 (en) 2011-08-22 2014-02-27 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono-and dioxides as BACE inhibitors, compositions and their use
US8338413B1 (en) 2012-03-07 2012-12-25 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070287692A1 (en) * 2006-06-12 2007-12-13 Yusheng Wu Aspartyl protease inhibitors

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
See also references of EP2485920A4 *
STACHEL ET AL.: "Structure-Besed Design Potent and Selective Cell-Pemeable inhibitors of Human Beta-Secretase (BACE-1).", JOURNAL OF MEDICINAL CHEMISTRY, vol. 47, 2004, pages 6447 - 6450 *

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8691831B2 (en) 2007-02-23 2014-04-08 Merck Sharp & Dohme Corp. Heterocyclic aspartyl protease inhibitors
US8653067B2 (en) 2007-04-24 2014-02-18 Shionogi & Co., Ltd. Pharmaceutical composition for treating Alzheimer's disease
US8637504B2 (en) 2008-06-13 2014-01-28 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
US9273053B2 (en) 2008-06-13 2016-03-01 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having Beta secretase inhibitory activity
US9145426B2 (en) 2011-04-07 2015-09-29 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
US9221839B2 (en) 2011-04-07 2015-12-29 Merck Sharp & Dohme Corp. C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
US9181236B2 (en) 2011-08-22 2015-11-10 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use

Also Published As

Publication number Publication date
WO2011044185A2 (en) 2011-04-14
EP2485920A4 (en) 2013-04-24
US8569310B2 (en) 2013-10-29
EP2485920A2 (en) 2012-08-15
EP2485920B1 (en) 2016-04-27
US20120195881A1 (en) 2012-08-02

Similar Documents

Publication Publication Date Title
WO2011044185A3 (en) Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
WO2009131974A8 (en) Thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as bace-1 inhibitors, compositions, and their use
MX2012004148A (en) Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use.
TR201906936T4 (en) Thienopyrimidine derivatives with inhibitory activity towards protein kinase.
EA201391786A1 (en) HALOGEN-ALKYL-1,3-OXAZINS AS BACE1 AND / OR BACE2 INHIBITORS
AU2012243329A8 (en) 5-substituted iminothiazines and their mono-and dioxides as BACE inhibitors,compositions,and their use
UA99141C2 (en) Substituted indazole derivatives active as kinase inhibitors
WO2009071480A3 (en) Substituted dihydropteridin-6-one derivatives, process for their preparation and their use as kinase inhibitors
DK2324008T3 (en) Diarylpyrazole as protein kinase inhibitors
BR112013014184A2 (en) triazine [1,2,4] triazolo [4,3-b] [1,2,4] compounds, method of preparation and their use
NO20092737L (en) Substituted pyrazoloquinazoline derivatives, process for their preparation and their use as kinase inhibitors
EA201101243A1 (en) 3H-IMIDAZO [4,5-C] PIRIDIN-6-CARBOXAMIDE AS ANTI-INFLAMMATORY MEANS
UA103272C2 (en) 2-amino-5,5-difluoro-5,6-dihydro-4h-[1,3]oxazines as bace1 and/or bace2 inhibitors
WO2007096151A3 (en) Inhibitors of p38-kinase for treatment of pulmonary hypertension
EA201391752A1 (en) SPYRO- [1,3] -OXAZINS AND SPYRO- [1,4] -OXAZEPINS AS BACE1 AND / OR BACE2 INHIBITORS
IN2014DN06101A (en)
WO2012104263A3 (en) 1,4 oxazines as bace1 and/or bace2 inhibitors
WO2010066684A3 (en) Pyridyloxyindoles inhibitors of vegf-r2 and use thereof for treatment of disease
EA201171306A1 (en) SUBSTITUTED IMIDAZO [1,2-α] PYRIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE AS β-SECRETASE INHIBITORS
SI2453923T1 (en) Peptide-mediated non-covalent delivery of active agents across the blood brain barrier
BRPI0810641A2 (en) "pharmaceutical compounds".
WO2011127333A3 (en) Compounds for treating disease, for administering, and for pharmaceutical compositions
EA201270535A1 (en) PURINE DERIVATIVES APPLICABLE AS HSP90 INHIBITORS
EA201201050A1 (en) PYRAZOLES AS AN ANTAGONISTS CRTH2
WO2009036996A3 (en) Small molecule bradykinin b1 receptor antagonists

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 10822570

Country of ref document: EP

Kind code of ref document: A1

WWE Wipo information: entry into national phase

Ref document number: 13391441

Country of ref document: US

NENP Non-entry into the national phase

Ref country code: DE

WWE Wipo information: entry into national phase

Ref document number: 2010822570

Country of ref document: EP